WO2014068587A3 - Procédé amélioré de synthèse du dabigatran et de ses intermédiaires - Google Patents

Procédé amélioré de synthèse du dabigatran et de ses intermédiaires Download PDF

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Publication number
WO2014068587A3
WO2014068587A3 PCT/IN2013/000652 IN2013000652W WO2014068587A3 WO 2014068587 A3 WO2014068587 A3 WO 2014068587A3 IN 2013000652 W IN2013000652 W IN 2013000652W WO 2014068587 A3 WO2014068587 A3 WO 2014068587A3
Authority
WO
WIPO (PCT)
Prior art keywords
synthesis
improved process
intermediates
dabigatran
formula
Prior art date
Application number
PCT/IN2013/000652
Other languages
English (en)
Other versions
WO2014068587A2 (fr
Inventor
Manik Reddy Pullagurla
Jagadeesh Babu Rangisetty
Mecheril Valsan Nandakumar
Original Assignee
Biophore India Pharmaceuticals Pvt. Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Biophore India Pharmaceuticals Pvt. Ltd. filed Critical Biophore India Pharmaceuticals Pvt. Ltd.
Priority to US14/438,995 priority Critical patent/US9533971B2/en
Publication of WO2014068587A2 publication Critical patent/WO2014068587A2/fr
Publication of WO2014068587A3 publication Critical patent/WO2014068587A3/fr
Priority to US15/291,087 priority patent/US10077251B2/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne un procédé amélioré de préparation du dabigatran étexilate (formule I), un sel pharmaceutiquement acceptable pour le traitement des thromboses, des maladies cardiovasculaires, etc., ainsi que des intermédiaires intervenant dans la synthèse. [Formule à insérer ici]
PCT/IN2013/000652 2012-10-29 2013-10-28 Procédé amélioré de synthèse du dabigatran et de ses intermédiaires WO2014068587A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US14/438,995 US9533971B2 (en) 2012-10-29 2013-10-28 Process for the synthesis of dabigatran and its intermediates
US15/291,087 US10077251B2 (en) 2012-10-29 2016-10-12 Process for the synthesis of Dabigatran Etexilate and its intermediates

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN4484CH2012 2012-10-29
IN4484/CHE/2012 2012-10-29

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US14/438,995 A-371-Of-International US9533971B2 (en) 2012-10-29 2013-10-28 Process for the synthesis of dabigatran and its intermediates
US15/291,087 Division US10077251B2 (en) 2012-10-29 2016-10-12 Process for the synthesis of Dabigatran Etexilate and its intermediates

Publications (2)

Publication Number Publication Date
WO2014068587A2 WO2014068587A2 (fr) 2014-05-08
WO2014068587A3 true WO2014068587A3 (fr) 2014-07-17

Family

ID=50628207

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2013/000652 WO2014068587A2 (fr) 2012-10-29 2013-10-28 Procédé amélioré de synthèse du dabigatran et de ses intermédiaires

Country Status (2)

Country Link
US (1) US9533971B2 (fr)
WO (1) WO2014068587A2 (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10077251B2 (en) * 2012-10-29 2018-09-18 Biophore India Pharmaceuticals Pvt. Ltd. Process for the synthesis of Dabigatran Etexilate and its intermediates
CN104744438A (zh) * 2014-12-17 2015-07-01 烟台东诚药业集团股份有限公司 一种用于合成制备达比加群酯苯并咪唑中间体的方法
CN105348263B (zh) * 2015-12-15 2018-03-23 乐普药业股份有限公司 一种达比加群酯中间体的制备方法
CN105906607A (zh) * 2015-12-23 2016-08-31 嘉实（湖南）医药科技有限公司 一种达比加群酯的合成方法
CN107417603B (zh) * 2017-05-17 2020-08-11 张家港威胜生物医药有限公司 一种克里唑替尼中间体制备方法
CN111793058A (zh) * 2019-04-09 2020-10-20 鲁南制药集团股份有限公司 一种制备达比加群酯中间体的改良方法

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998037075A1 (fr) * 1997-02-18 1998-08-27 Boehringer Ingelheim Pharma Kg Heterocycles bicycliques disubstitues, production et utilisation comme medicaments
WO2000001704A2 (fr) * 1998-07-04 2000-01-13 Boehringer Ingelheim Pharma Kg Benzimidazoles, leur preparation et leur utilisation comme medicaments
DE19962329A1 (de) * 1999-12-23 2001-06-28 Boehringer Ingelheim Pharma Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
US20030004356A1 (en) * 1999-12-23 2003-01-02 Boehringer Ingelheim Pharma Kg Benzimidazoles with antithrombotic activity
WO2006000353A1 (fr) * 2004-06-25 2006-01-05 Boehringer Ingelheim International Gmbh Procede pour produire des 4-(benzimidazolylmethylamino)-benzamidines
WO2007071743A1 (fr) * 2005-12-21 2007-06-28 Boehringer Ingelheim International Gmbh Procede ameliore pour la preparation de sels de 4-(benzimidazolylmethylamino)-benzamides
WO2007071742A1 (fr) * 2005-12-21 2007-06-28 Boehringer Ingelheim International Gmbh Procede ameliore pour la preparation de 4-(benzimidazolylmethylamino)-benzamides et des sels de ceux-ci
WO2008095928A1 (fr) * 2007-02-06 2008-08-14 Boehringer Ingelheim International Gmbh Procédé de préparation d'un dérivé de benzimidazole
WO2009111997A1 (fr) * 2008-03-14 2009-09-17 Zentiva, K.S. Procédé de préparation de dabigatran
WO2009153214A1 (fr) * 2008-06-16 2009-12-23 Boehringer Ingelheim International Gmbh Procédé de fabrication d'un intermédiaire dans la synthèse du dabigatran
WO2012004397A1 (fr) * 2010-07-09 2012-01-12 Esteve Química, S.A. Intermédiaires et procédé de préparation d'un inhibiteur spécifique de la thrombine
WO2013111163A2 (fr) * 2012-01-20 2013-08-01 Cadila Healthcare Limited Procédé de préparation de dabigatran étéxilate mésylate et polymorphes d'intermédiaires de celui-ci

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998037075A1 (fr) * 1997-02-18 1998-08-27 Boehringer Ingelheim Pharma Kg Heterocycles bicycliques disubstitues, production et utilisation comme medicaments
WO2000001704A2 (fr) * 1998-07-04 2000-01-13 Boehringer Ingelheim Pharma Kg Benzimidazoles, leur preparation et leur utilisation comme medicaments
DE19962329A1 (de) * 1999-12-23 2001-06-28 Boehringer Ingelheim Pharma Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
US20030004356A1 (en) * 1999-12-23 2003-01-02 Boehringer Ingelheim Pharma Kg Benzimidazoles with antithrombotic activity
WO2006000353A1 (fr) * 2004-06-25 2006-01-05 Boehringer Ingelheim International Gmbh Procede pour produire des 4-(benzimidazolylmethylamino)-benzamidines
WO2007071743A1 (fr) * 2005-12-21 2007-06-28 Boehringer Ingelheim International Gmbh Procede ameliore pour la preparation de sels de 4-(benzimidazolylmethylamino)-benzamides
WO2007071742A1 (fr) * 2005-12-21 2007-06-28 Boehringer Ingelheim International Gmbh Procede ameliore pour la preparation de 4-(benzimidazolylmethylamino)-benzamides et des sels de ceux-ci
WO2008095928A1 (fr) * 2007-02-06 2008-08-14 Boehringer Ingelheim International Gmbh Procédé de préparation d'un dérivé de benzimidazole
WO2009111997A1 (fr) * 2008-03-14 2009-09-17 Zentiva, K.S. Procédé de préparation de dabigatran
WO2009153214A1 (fr) * 2008-06-16 2009-12-23 Boehringer Ingelheim International Gmbh Procédé de fabrication d'un intermédiaire dans la synthèse du dabigatran
WO2012004397A1 (fr) * 2010-07-09 2012-01-12 Esteve Química, S.A. Intermédiaires et procédé de préparation d'un inhibiteur spécifique de la thrombine
WO2013111163A2 (fr) * 2012-01-20 2013-08-01 Cadila Healthcare Limited Procédé de préparation de dabigatran étéxilate mésylate et polymorphes d'intermédiaires de celui-ci

Also Published As

Publication number Publication date
WO2014068587A2 (fr) 2014-05-08
US9533971B2 (en) 2017-01-03
US20150246900A1 (en) 2015-09-03

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